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576 results

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Discovering cell-active BCL6 inhibitors: effectively combining biochemical HTS with multiple biophysical techniques, X-ray crystallography and cell-based assays.
Pierrat OA, Liu M, Collie GW, Shetty K, Rodrigues MJ, Le Bihan YV, Gunnell EA, McAndrew PC, Stubbs M, Rowlands MG, Yahya N, Shehu E, Talbot R, Pickard L, Bellenie BR, Cheung KJ, Drouin L, Innocenti P, Woodward H, Davis OA, Lloyd MG, Varela A, Huckvale R, Broccatelli F, Carter M, Galiwango D, Hayes A, Raynaud FI, Bryant C, Whittaker S, Rossanese OW, Hoelder S, Burke R, van Montfort RLM. Pierrat OA, et al. Among authors: whittaker s. Sci Rep. 2022 Nov 3;12(1):18633. doi: 10.1038/s41598-022-23264-z. Sci Rep. 2022. PMID: 36329085 Free PMC article.
Development of novel, highly potent inhibitors of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF): increasing cellular potency through optimization of a distal heteroaromatic group.
Suijkerbuijk BM, Niculescu-Duvaz I, Gaulon C, Dijkstra HP, Niculescu-Duvaz D, Ménard D, Zambon A, Nourry A, Davies L, Manne HA, Friedlos F, Ogilvie LM, Hedley D, Lopes F, Preece NP, Moreno-Farre J, Raynaud FI, Kirk R, Whittaker S, Marais R, Springer CJ. Suijkerbuijk BM, et al. Among authors: whittaker s. J Med Chem. 2010 Apr 8;53(7):2741-56. doi: 10.1021/jm900607f. J Med Chem. 2010. PMID: 20199087
Pyridoimidazolones as novel potent inhibitors of v-Raf murine sarcoma viral oncogene homologue B1 (BRAF).
Niculescu-Duvaz D, Gaulon C, Dijkstra HP, Niculescu-Duvaz I, Zambon A, Ménard D, Suijkerbuijk BM, Nourry A, Davies L, Manne H, Friedlos F, Ogilvie L, Hedley D, Whittaker S, Kirk R, Gill A, Taylor RD, Raynaud FI, Moreno-Farre J, Marais R, Springer CJ. Niculescu-Duvaz D, et al. Among authors: whittaker s. J Med Chem. 2009 Apr 23;52(8):2255-64. doi: 10.1021/jm801509w. J Med Chem. 2009. PMID: 19323560
Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors.
Wilson SC, Atrash B, Barlow C, Eccles S, Fischer PM, Hayes A, Kelland L, Jackson W, Jarman M, Mirza A, Moreno J, Nutley BP, Raynaud FI, Sheldrake P, Walton M, Westwood R, Whittaker S, Workman P, McDonald E. Wilson SC, et al. Among authors: whittaker s. Bioorg Med Chem. 2011 Nov 15;19(22):6949-65. doi: 10.1016/j.bmc.2011.08.051. Epub 2011 Aug 31. Bioorg Med Chem. 2011. PMID: 21982796
In vitro and in vivo pharmacokinetic-pharmacodynamic relationships for the trisubstituted aminopurine cyclin-dependent kinase inhibitors olomoucine, bohemine and CYC202.
Raynaud FI, Whittaker SR, Fischer PM, McClue S, Walton MI, Barrie SE, Garrett MD, Rogers P, Clarke SJ, Kelland LR, Valenti M, Brunton L, Eccles S, Lane DP, Workman P. Raynaud FI, et al. Among authors: whittaker sr. Clin Cancer Res. 2005 Jul 1;11(13):4875-87. doi: 10.1158/1078-0432.CCR-04-2264. Clin Cancer Res. 2005. PMID: 16000586
Novel hinge binder improves activity and pharmacokinetic properties of BRAF inhibitors.
Zambon A, Ménard D, Suijkerbuijk BM, Niculescu-Duvaz I, Whittaker S, Niculescu-Duvaz D, Nourry A, Davies L, Manne HA, Lopes F, Preece N, Hedley D, Ogilvie LM, Kirk R, Marais R, Springer CJ. Zambon A, et al. Among authors: whittaker s. J Med Chem. 2010 Aug 12;53(15):5639-55. doi: 10.1021/jm100383b. J Med Chem. 2010. PMID: 20597484
576 results